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Anti-microbial Effects In Vitro and In Vivo of Alstonia scholaris.

ABSTRACT: Alstonia scholaris could be used as a traditional medicinal plant in China for the treatment of acute respiratory, which might be caused by respiratory tract infections. The investigation tested the anti-infective effects of total alkaloids extract (TA) from leaves of A. scholaris, and as a result, TA inhibited herpes simplex virus type 1 (HSV-1), respiratory syncytial virus (RSV) and influenza A virus (H1N1) in vitro respectively. In addition, the survival days of mice were prolonged, and the lung weights and mortality of mice were decreased significantly, after oral administrated TA in H1N1 and beta-hemolytic streptococcus infectious models in vivo respectively. The finding supported partly the traditional usage of A. scholaris in the treatment of respiratory infections.

SUBMITTER: Zhao YL

PROVIDER: S-EPMC7778864 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature

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Anti-microbial Effects In Vitro and In Vivo of Alstonia scholaris.

Zhao Yun-Li YL Gou Zhong-Ping ZP Shang Jian-Hua JH Li Wan-Yi WY Kuang Yu Y Li Ming-Yuan MY Luo Xiao-Dong XD

Natural products and bioprospecting 20210103 1

Alstonia scholaris could be used as a traditional medicinal plant in China for the treatment of acute respiratory, which might be caused by respiratory tract infections. The investigation tested the anti-infective effects of total alkaloids extract (TA) from leaves of A. scholaris, and as a result, TA inhibited herpes simplex virus type 1 (HSV-1), respiratory syncytial virus (RSV) and influenza A virus (H1N1) in vitro respectively. In addition, the survival days of mice were prolonged, and the l ...[more]

PMID: 33389714

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Alstonia scholaris

Project description:Alstonia scholaris overview

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Alstonia scholaris

Project description:De novo transcriptome analysis of Alstonia scholaris for decoding indole alkaloids biosynthetic genes involved in pathway

| PRJNA1008869 | ENA

Antiviral Cystine Knot α-Amylase Inhibitors from Alstonia scholaris.

Project description:Cystine knot α-amylase inhibitors are cysteine-rich, proline-rich peptides found in the Amaranthaceae and Apocynaceae plant species. They are characterized by a pseudocyclic backbone with two to four prolines and three disulfides arranged in a knotted motif. Similar to other knottins, cystine knot α-amylase inhibitors are highly resistant to degradation by heat and protease treatments. Thus far, only the α-amylase inhibition activity has been described for members of this family. Here, we show that cystine knot α-amylase inhibitors named alstotides discovered from the Alstonia scholaris plant of the Apocynaceae family display antiviral activity. The alstotides (As1-As4) were characterized by both proteomic and genomic methods. All four alsotides are novel, heat-stable and enzyme-stable and contain 30 residues. NMR determination of As1 and As4 structures reveals their conserved structural fold and the presence of one or more cis-proline bonds, characteristics shared by other cystine knot α-amylase inhibitors. Genomic analysis showed that they contain a three-domain precursor, an arrangement common to other knottins. We also showed that alstotides are antiviral and cell-permeable to inhibit the early phase of infectious bronchitis virus and Dengue infection, in addition to their ability to inhibit α-amylase. Taken together, our results expand membership of cystine knot α-amylase inhibitors in the Apocynaceae family and their bioactivity, functional promiscuity that could be exploited as leads in developing therapeutics.

| S-EPMC4692237 | biostudies-literature

Monoterpenoid Indole Alkaloids from Inadequately Dried Leaves of Alstonia scholaris.

Project description:Six new indole alkaloids, named alstoniascholarines L-Q (1-6), together with nineteen known analogues were isolated from the inadequately dried leaves of Alstonia scholaris. Their structures were elucidated on the basis of extensive analysis of spectroscopic data and by comparison of their physical and spectroscopic data with the literature values. In addition, the new alkaloids were tested for their cytotoxic and neurite outgrowth-promoting activities.

| S-EPMC4567994 | biostudies-literature

Antibacterial and Synergistic Activity of Pentacyclic Triterpenoids Isolated from Alstonia scholaris.

Project description:(1) BACKGROUND: Alstonia scholaris (Apocynaceae) is an important medicinal plant that has been historically used in "Dai" ethnopharmacy to treat infectious diseases in China. Although various pharmacological activities have been reported, the antimicrobial constitutes of A. scholaris have not yet been identified. The objective of this study is to evaluate the antibacterial constitutes from the leaf extract of A. scholaris and to assess the synergistic effects of isolated compounds with antibiotics against bacterial pathogens.; (2) METHODS: The chemical constitutes isolated from the leaf extract of A. scholaris were structurally identified by NMR. The antibacterial and synergistic effect of compounds was assessed by calculating the minimal inhibitory concentration (MIC), checkerboard dilution test, and time-kill assay.; (3) RESULTS: Six pentacyclic triterpenoids were structurally identified as (1) lupeol, (2) betulin, (3) 3-hydroxy-11-ursen-28,13-olide, (4) betulinic acid, (5) oleanolic acid and (6) ursolic acid. Both oleanolic and ursolic acid showed antibacterial activity but were limited to Gram-positive bacteria. Ursolic acid showed a synergistic effect with ampicillin and tetracycline against both Bacillus cereus and S. aureus.; (4) CONCLUSION: These findings reflect that pentacyclic triterpenoids are the antibacterial chemicals in A. scholaris. The ability of ursolic acid to enhance the activity of antibiotics can constitute a valuable group of therapeutic agents in the future.

| S-EPMC6273878 | biostudies-literature

In-vitro antigout potential of Alstonia scholaris flower, characterization and prospective ligand-receptor interaction of bioactive lead compound.

Project description:Gout is an arthropathic and inflammatory disease. The prevalence and incidence of such disease has risen in last decades. It is associated with life style thus it could be recognize as life style diseases. In the present study, the flower extract of Alstonia scholaris Linn R.Br., Flower was initially subjected to extraction, isolation which leads to purification of pure eight compounds. All these compounds were identified using various spectroscopic techniques. In-vitro Xanthine oxidase inhibition activity was performed to determine the antigout potential of lead compounds. Compound 8 showed significant activity among all i.e. 14.7 ± 0.43 as compare to standard allopurinol 6.77 ± 0.26. Accordingly, in-silico studies using Autodock vina 4 showed the ligand-protein interaction of luteolin with 3AX7. The docking simulations showed significant binding pocket sites of respective proteins 3AX7 with the least binding energy -10.2 kcal/mol. Consequently, molecular docking simulations for 100ns indicated robust evidence with their conformational structural interaction which serve as active sites for Lead compound. Principal Component Analysis indicated first three PCs capture 23.8%, 39%, and 49% of structural variance in protein. Therefore compound 8 could be consider for potential drug design and development in gout therapy.

| S-EPMC10009449 | biostudies-literature

Complete plastome of the medicinally important plant, Alstonia scholaris (Apocynaceae).

Project description:Alstonia scholaris is an evergreen tropical tree with significant medicinal values. To better understand its genetic and genomic profiles, we sequenced and assembled the completed plastome of A. scholaris. The plastome is 154,699 bp in length, consisting of a large (LSC, 85,364 bp) and a small single-copy region (SSC, 18,027 bp), which are separated by a pair of inverted repeat regions (IRs, 25,654 bp). It possesses 116 unique genes (82 protein-coding genes, 30 tRNAs, and 4 rRNAs). Phylogenetic analysis suggests that A. scholaris is sister to the clade including remaining Apocynaceae species.

| S-EPMC7706523 | biostudies-literature

Assessment of Tissue Specific Distribution and Seasonal Variation of Alkaloids in Alstonia scholaris.

Project description:Alstonia scholaris is a well-known source of alkaloids and widely recognized for therapeutic purposes to treat the ailments in human and livestock. However, the composition and production of alkaloids vary due to tissue specific metabolism and seasonal variation. This study investigated alkaloids in leaves, stems, trunk barks, fruits, and flowers of A. scholaris. The impact of seasonal changes on the production of alkaloids in the leaves of A. scholaris was also investigated. One and two-dimensional Nuclear Magnetic Resonance (NMR) experiments were utilized for the characterization of alkaloids and total eight alkaloids (picrinine, picralinal, akuammidine, 19 S scholaricine, 19,20 E vallesamine, Nb-demethylalstogustine N-Oxide, Nb-demethylalstogustine, and echitamine) were characterized and quantified. Quantitative and multivariate analysis suggested that the alkaloids content is tissue specific, illustrating the effect of plant tissue organization on alkaloidal production in A. scholaris. The results suggest that the best part to obtain alkaloids is trunk barks, since it contains 7 alkaloids. However, the best part for isolating picrinine, picralinal, akuammidine, 19 S scholaricine, and 19,20 E vallesamine is fruit, since it shows highest amount of these alkaloids. Undoubtedly, NMR and statistical methods are very helpful to differentiate the profile of alkaloids in A. scholaris.

| S-EPMC9319449 | biostudies-literature

Genotoxicity and Safety Pharmacology Studies of Indole Alkaloids Extract from Leaves of Alstonia scholaris (L.) R. Br.

Project description:Indole alkaloids extract (IAAS) was prepared from leaves of Alstonia scholaris (L.) R. Br., an evergreen tropical plant widely distributed throughout the world. This plant has been used historically by the Dai ethnic people of China to treat respiratory diseases. This study evaluated the genotoxicity and safety pharmacology of IAAS to support clinical use. The bacterial reverse mutation (Ames) test, in vitro mammalian chromosomal aberration test, and in vivo mammalian erythrocyte micronucleus (MN) test were performed to evaluate genotoxicity. Mice were administered IAAS (240, 480, or 960 mg/kg bw) once orally to observe adverse central nervous system effects. Furthermore, beagle dogs were administered IAAS (10, 30, 60 mg/kg bw) once via the duodenum to evaluate its effects on the cardiovascular and respiratory systems. IAAS with or without S9-induced metabolic activation showed no genotoxicity in the Ames test up to 500 μg/plate, in the mammalian chromosomal aberration test up to 710 μg/mL, or in the MN test up to 800 mg/kg bw. No abnormal neurobehavioral effects were observed in mice following treatment with up to 960 mg/kg bw of IAAS. Moreover, blood pressure, heart rate, electrocardiogram parameters, and depth and rate of breathing in anesthetized beagle dogs did not differ among the IAAS doses or from the vehicle group. These data indicated that IAAS did not induce mutagenicity, clastogenicity, or genotoxicity, and no pharmaco-toxicological effects were observed in the respiratory, cardiovascular, or central nervous systems. Our results increased understanding of safety considerations associated with IAAS, and may indicate that IAAS is a possible drug candidate.

| S-EPMC7253540 | biostudies-literature

Acute and Chronic Toxicity of Indole Alkaloids from Leaves of Alstonia scholaris (L.) R. Br. in Mice and Rats.

Project description:Alstonia scholaris (L.) R. Br. (Apocynaceae) is an evergreen tree that has been used to treat lung diseases. In this study, the toxicity profile of indole alkaloids from leaves of A. scholaris was investigated. In acute toxicity tests, mice were administered total alkaloids (TA) and five indole alkaloids. In a chronic toxicity test, rats were continuously administered TA (50, 100, and 300 mg/kg bw) for 13 weeks, followed by a 4-week recovery. A single administration of TA affected the behavior of mice, and at 12.8 g/kg bw, prone position, shortness of breath, wheezing, and convulsion were observed. The half-lethal dose (LD50) in mice was 5.48 g/kg bw, almost 2740 times the clinical dose in humans. Among the five indole alkaloids, the maximum tolerance dose in mice ranged from 0.75 to 4 g/kg bw. The TA-treated rats did not die and showed no adverse effects or dose-dependent changes in weight or food and water consumption, despite fluctuations in hematological and biochemical parameters compared with historical data. Furthermore, both gross and histopathological observations revealed no abnormalities in any organ. With daily oral administration to rats, the non-observed-adverse-effect-level of TA was 100 mg/kg bw. The results indicate that TA is safe for clinical use.

| S-EPMC7176796 | biostudies-literature

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